Doxylamine
Doxylamine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Doxylamine
ATX code: R06AA09
Active ingredient: doxylamine (Doxylamine)
Manufacturer: NPO PharmVILAR LLC (Russia)
Description and photo update: 2020-17-07
Doxylamine is a hypnotic drug; antagonist of histamine H 1 receptors.
Release form and composition
Dosage form - tablets, film-coated: biconvex, oblong, with rounded ends, a dividing line is applied on one side, a film shell and an inner layer on a cross section - from white to almost white (10 pcs. In blisters made of polyvinyl chloride film and aluminum lacquered printing foil, in a cardboard box 1, 2, 3 or 4 cell packages and instructions for the use of Doxylamine).
Composition for 1 tablet:
- active ingredient: doxylamine succinate - 15 mg;
- auxiliary ingredients: lactose monohydrate - 50 mg; aerosil (colloidal silicon dioxide) - 0.5 mg; MCC (microcrystalline cellulose) - 27.7 mg; croscarmellose sodium - 5 mg; magnesium stearate - 1 mg; polyvinylpyrrolidone K-17 - 0.8 mg;
- film shell: white Opadray II 85F48105 (polyvinyl alcohol - 46.9%; macrogol-3350 - 23.6%; titanium dioxide - 12.1%; talc - 17.4%) - 3 mg.
Pharmacological properties
Pharmacodynamics
The active ingredient of the drug is doxylamine, is a blocker of H 1 -histamine receptors, belongs to the group of ethanolamines. It has hypnotic, sedative, antihistamine and m-anticholinergic effects. Reduces the period of falling asleep, increases the duration and quality of sleep, does not affect the phases of sleep.
The duration of the product is from 6 to 8 hours.
Pharmacokinetics
The main pharmacokinetic parameters of doxylamine:
- absorption: after oral administration, doxylamine is absorbed to a high degree, the maximum concentration (C max) in the blood plasma on average reaches after 2 hours;
- metabolism and distribution: biotransformation of the substance occurs in the liver; it penetrates well through the histohematological barriers, including through the blood-brain barrier;
- excretion: T 1/2 (half-life) of doxylamine is about 10 hours. It is excreted unchanged: mainly by the kidneys - up to 60%, partially - through the digestive tract.
In renal / hepatic failure, as well as in elderly patients, it is possible to lengthen T 1/2 of doxylamine.
After repeated administration of the drug, the equilibrium concentration of doxylamine and its metabolites in the blood plasma reach later and at a higher level.
Indications for use
Doxylamine is used to treat transient sleep disorders.
Contraindications
Absolute:
- diseases of the urethra and prostate, accompanied by a violation of the outflow of urine;
- angle-closure glaucoma (including family history of the disease);
- lack of lactase, lactose intolerance, glucose-galactose malabsorption;
- children and adolescents under 15 years old;
- lactation period;
- established hypersensitivity to doxylamine, other antihistamines and / or auxiliary components of the drug.
Under medical supervision, the drug should be used in patients with a history of apnea episodes, since doxylamine can aggravate the syndrome of sudden respiratory arrest during sleep (sleep apnea), as well as in renal and hepatic insufficiency, since these diseases can increase T 1/2 of the drug.
Caution when taking Doxylamine should be observed by patients over 65 years of age: side effects in the form of dizziness and slowing down reactions are fraught with falls, for example, during nighttime awakenings after taking sleeping pills. In addition, older people are more likely to increase T 1/2.
Doxylamine, instructions for use: method and dosage
Doxylamine tablets are taken 15-30 minutes before bedtime, drinking plenty of fluids.
The recommended daily dose for children over 15 years of age and adults is 0.5 or 1 tablet (7.5 or 15 mg) per dose.
In the absence of a pronounced therapeutic effect, after agreement with the doctor, the daily dose can be increased to 2 tablets (30 mg) per dose.
The duration of the course is 2–5 days. If insomnia persists, consult a doctor.
Side effects
When Doxylamine is taken from the side of human systems and organs, the following adverse reactions may develop:
- gastrointestinal tract: dry mouth, constipation;
- nervous system: daytime sleepiness (requires dose reduction), hallucinations, confusion;
- organ of vision: blurred vision, impaired accommodation of the eye, blurred vision;
- cardiovascular system: palpitations;
- kidneys and urinary tract: urinary retention;
- musculoskeletal system: rhabdomyolysis;
- laboratory indicators: an increase in the concentration of CPK (creatine phosphokinase).
In case of aggravation of any of these adverse reactions or the development of other side effects not noted in the instructions, a doctor's consultation is necessary.
Overdose
Symptoms of an overdose of doxylamine are agitation, daytime sleepiness, disturbances in the accommodation of the eye, mydriasis (dilation of the pupil), dry mouth, hyperemia of the vessels of the skin of the face and neck, hyperthermia (increased body temperature), sinus tachycardia, hallucinations, disturbance of consciousness, lability of mood, anxiety, tremor, impaired coordination of movements, athetosis (involuntary movements of fingers and toes), convulsive syndrome, coma.
In some cases, involuntary movements can be harbingers of seizures, which indicates a severe degree of intoxication. But even the absence of seizures in severe doxylamine poisoning does not exclude the possibility of rhabdomyolysis, which is often accompanied by acute renal failure. Such patients are shown standard treatment with constant monitoring of the concentration of CPK in the blood serum.
The appearance of these symptoms of an overdose requires an urgent visit to a specialist.
As a first aid for the ingestion of high doses of doxylamine, the use of activated charcoal in a single dose for adults - 50 g, for children - 1 g / kg of body weight is indicated. In the future, symptomatic therapy is carried out, including m-cholinomimetics and other drugs according to indications.
special instructions
It is important to consider that sleep disorders can occur for various reasons, including those that do not require drug therapy.
Taking Doxylamine has a sedative effect on the patient, inhibits cognitive abilities, and also slows down his psychomotor reactions.
Antihistamines of the 1st generation are capable of exerting m-anticholinergic, anti-α-adrenergic and antiserotonin effects, which may result in dry mouth, urinary retention, constipation, impaired eye accommodation and visual impairment.
Like all drugs with a hypnotic or sedative effect, Doxylamine increases the risk of sleep apnea syndrome (sudden stopping of breathing during sleep) and increases the number and duration of apnea attacks.
Patients with rare genetic diseases - Lapp lactase deficiency, severe galactose intolerance, glucose-galactose malabsorption - should take into account that 1 tablet of Doxylamine contains lactose monohydrate in an amount of 50 mg.
Influence on the ability to drive vehicles and complex mechanisms
Taking the drug at night can cause drowsiness in the patient during the daytime, and therefore driving vehicles, working with complex mechanisms and performing other activities that require increased concentration of attention and high speed of psychomotor reactions should be avoided.
Application during pregnancy and lactation
In the course of adequate and well-controlled clinical studies, it has been confirmed that doxylamine can be used by pregnant women throughout the entire period of gestation. But when prescribing the drug in late pregnancy, it is necessary to take into account the likelihood of an atropine-like and sedative effect of the substance on the condition of the newborn.
There is no reliable data on the penetration of doxylamine into a woman's breast milk. In this regard, given the possibility of the sedative and stimulating effect of the substance on the child, if it is necessary to use the drug during lactation, breastfeeding should be abandoned.
Pediatric use
In pediatric practice, the use of Doxylamine tablets is contraindicated for the treatment of children and adolescents under 15 years of age.
With impaired renal function
Patients with renal insufficiency, given the data on an increase in the level of doxylamine in the blood plasma and a decrease in its plasma clearance, may require dose adjustment downward.
For violations of liver function
Patients with hepatic impairment, given the data on an increase in the level of doxylamine in the blood plasma and a decrease in its plasma clearance, may require a dose adjustment downward.
Use in the elderly
Elderly patients (over 65 years old) blockers of H 1 -histamine receptors, including doxylamine, should be taken with caution. The likelihood of developing dizziness and slowing reactions is associated with the risk of falls and injury, for example, during nighttime awakenings after the use of sleeping pills.
Given the data on an increase in the level of a substance in the blood plasma and a decrease in its plasma clearance in this group of patients, it may be necessary to adjust the dose of the drug downward.
Drug interactions
- sedative antidepressants (amitriptyline, doxepin, mirtazapine, mianserin, trimipramine), benzodiazepines, barbiturates, clonidine, morphine derivatives (antitussive drugs, analgesics), antipsychotics, anxiolytics, sedative actions Non- 1- antihistamines, antigistamines, central antihistamines: when used simultaneously with Doxylamine, their depressing effect on the central nervous system is enhanced;
- m-anticholinergics (atropine, imipramine antidepressants, antiparkinsonian drugs, atropine antispasmodics, disopyramide, antipsychotics of the phenothiazine series): doxylamine increases the risk of developing such adverse reactions as constipation, urinary retention, dry mouth;
- ethanol: alcohol potentiates the sedative effect of most H 1 blockers - histamine receptors, including Doxylamine; during therapy, it is necessary to avoid the simultaneous use of drugs containing ethanol and the use of alcoholic beverages.
Analogs
Doxylamine analogues are Andante, Valocordin-Doxylamin, Hypnogen, Doxylamin-SZ, Donormil, Zolpidem, Imovan, Nitrazepam, Oniria, Reslip, Slipzon, Somnol, Thorson, Tsirkadin, etc.
Terms and conditions of storage
Store at a temperature not exceeding + 25 ° С in a place inaccessible to children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Doxylamine
There are no reviews of Doxylamine produced by NPO PharmVILAR on the available medical resources. All patients respond extremely positively to sleeping pills containing the substance of the same name as an active ingredient. It is said to be the most effective remedy for problems with falling asleep and / or sleep duration, with little or no adverse reactions.
The price of Doxylamine in pharmacies
The price of Doxylamine is currently unknown as the drug is not available for sale.
The approximate cost of direct analogs, the active ingredient of which is doxylamine, in the form of film-coated tablets, per package 30 pcs. is: Reslip - 325 rubles; Slipzon - from 273 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
